Peringatan Keamanan

Bosentan has been given as a single dose of up to 2400 mg in normal volunteers, or up to 2000 mg/day for 2 months in patients, without any major clinical consequences. The most common side effect was headache of mild to moderate intensity. In the cyclosporine A interaction study, in which doses of 500 and 1000 mg b.i.d. of bosentan were given concomitantly with cyclosporine A, trough plasma concentrations of bosentan increased 30-fold, resulting in severe headache, nausea, and vomiting, but no serious adverse events. Mild decreases in blood pressure and increases in heart rate were observed. There is no specific experience of overdosage with bosentan beyond the doses described above. Massive overdosage may result in pronounced hypotension requiring active cardiovascular support.

Bosentan

DB00559

small molecule approved investigational

Deskripsi

Bosentan is a dual endothelin receptor antagonist marketed under the trade name Tracleer by Actelion Pharmaceuticals. Bosentan is used to treat pulmonary hypertension by blocking the action of endothelin molecules that would otherwise promote narrowing of the blood vessels and lead to high blood pressure.

Struktur Molekul 2D

Berat 551.614
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal elimination half-life is about 5 hours in healthy adult subjects.
Volume Distribusi * 18 L
Klirens (Clearance) * 4 L/h [patients with pulmonary arterial hypertension]

Absorpsi

Absolute bioavailability is approximately 50% and food does not affect absorption.

Metabolisme

Bosentan is metabolized in the liver by the cytochrome P450 enzymes CYP2C9 and CYP3A4 (and possibly CYP2C19), producing three metabolites, one of which, Ro 48-5033, is pharmacologically active and may contribute 10 to 20% to the total activity of the parent compound.

Rute Eliminasi

Bosentan is eliminated by biliary excretion following metabolism in the liver.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1239 Data
Cyclosporine The serum concentration of Bosentan can be increased when it is combined with Cyclosporine.
Glycochenodeoxycholic Acid Bosentan may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Fluvoxamine Bosentan may decrease the excretion rate of Fluvoxamine which could result in a higher serum level.
Glimepiride Bosentan may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Isradipine Bosentan may decrease the excretion rate of Isradipine which could result in a higher serum level.
Flucloxacillin Bosentan may decrease the excretion rate of Flucloxacillin which could result in a higher serum level.
Indomethacin Bosentan may decrease the excretion rate of Indomethacin which could result in a higher serum level.
Atenolol Bosentan may decrease the excretion rate of Atenolol which could result in a higher serum level.
Rosiglitazone Bosentan may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Spironolactone Spironolactone may increase the hypotensive activities of Bosentan.
Cerivastatin Bosentan may decrease the excretion rate of Cerivastatin which could result in a higher serum level.
Loratadine Bosentan may decrease the excretion rate of Loratadine which could result in a higher serum level.
Atropine Bosentan may decrease the excretion rate of Atropine which could result in a higher serum level.
Diclofenac Bosentan may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Losartan The metabolism of Losartan can be increased when combined with Bosentan.
Fluorescein Bosentan may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin Bosentan may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Naproxen Bosentan may decrease the excretion rate of Naproxen which could result in a higher serum level.
Disulfiram Bosentan may decrease the excretion rate of Disulfiram which could result in a higher serum level.
Cefaclor Bosentan may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Tinidazole Bosentan may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Repaglinide Bosentan may decrease the excretion rate of Repaglinide which could result in a higher serum level.
Telmisartan Bosentan may decrease the excretion rate of Telmisartan which could result in a higher serum level.
Ezetimibe Bosentan may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Dipyridamole Bosentan may decrease the excretion rate of Dipyridamole which could result in a higher serum level.
Sulfamethoxazole Bosentan may decrease the excretion rate of Sulfamethoxazole which could result in a higher serum level.
Fenofibrate Bosentan may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Nitrendipine Bosentan may decrease the excretion rate of Nitrendipine which could result in a higher serum level.
Glipizide Bosentan may decrease the excretion rate of Glipizide which could result in a higher serum level.
Sulfinpyrazone Bosentan may decrease the excretion rate of Sulfinpyrazone which could result in a higher serum level.
Ofloxacin Bosentan may decrease the excretion rate of Ofloxacin which could result in a higher serum level.
Taurocholic acid Bosentan may decrease the excretion rate of Taurocholic acid which could result in a higher serum level.
Prasterone sulfate Bosentan may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Indocyanine green acid form Bosentan may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone Bosentan may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Pilsicainide Bosentan may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Dihydroergocristine Bosentan may decrease the excretion rate of Dihydroergocristine which could result in a higher serum level.
Glycyrrhizic acid Bosentan may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Nifedipine Bosentan may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Budesonide Bosentan may decrease the excretion rate of Budesonide which could result in a higher serum level.
Belantamab mafodotin Bosentan may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Bosentan.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Bosentan.
Alfuzosin Alfuzosin may increase the hypotensive activities of Bosentan.
Amifostine Bosentan may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Bosentan.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Bosentan.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Bosentan.
Obinutuzumab Bosentan may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Bosentan.
Rituximab Bosentan may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Bosentan.
Midodrine Midodrine may decrease the antihypertensive activities of Bosentan.
Isoetharine Isoetharine may decrease the antihypertensive activities of Bosentan.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Bosentan.
Etomidate Etomidate may decrease the antihypertensive activities of Bosentan.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Bosentan.
Protriptyline Protriptyline may decrease the antihypertensive activities of Bosentan.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Bosentan.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Bosentan.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Bosentan.
Droperidol Droperidol may decrease the antihypertensive activities of Bosentan.
Amoxapine Amoxapine may decrease the antihypertensive activities of Bosentan.
Doxapram Doxapram may decrease the antihypertensive activities of Bosentan.
Metaraminol Metaraminol may decrease the antihypertensive activities of Bosentan.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Bosentan.
Nicergoline Nicergoline may decrease the antihypertensive activities of Bosentan.
Methoxamine Methoxamine may decrease the antihypertensive activities of Bosentan.
Propiomazine Propiomazine may decrease the antihypertensive activities of Bosentan.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Bosentan.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Bosentan.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Bosentan.
Dobutamine Dobutamine may decrease the antihypertensive activities of Bosentan.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Bosentan.
Ritodrine Ritodrine may decrease the antihypertensive activities of Bosentan.
Terbutaline Terbutaline may decrease the antihypertensive activities of Bosentan.
Flupentixol Flupentixol may decrease the antihypertensive activities of Bosentan.
Bitolterol Bitolterol may decrease the antihypertensive activities of Bosentan.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Bosentan.
Naratriptan Naratriptan may decrease the antihypertensive activities of Bosentan.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Bosentan.
Dopamine Dopamine may decrease the antihypertensive activities of Bosentan.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Bosentan.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Bosentan.
Arbutamine Arbutamine may decrease the antihypertensive activities of Bosentan.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Bosentan.
Fenoterol Fenoterol may decrease the antihypertensive activities of Bosentan.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Bosentan.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Bosentan.
Ephedrine Ephedrine may decrease the antihypertensive activities of Bosentan.
Mephentermine Mephentermine may decrease the antihypertensive activities of Bosentan.
Procaterol Procaterol may decrease the antihypertensive activities of Bosentan.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Bosentan.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Bosentan.
Bambuterol Bambuterol may decrease the antihypertensive activities of Bosentan.
MMDA MMDA may decrease the antihypertensive activities of Bosentan.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Bosentan.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Bosentan.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Bosentan.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Bosentan.

Target Protein

Endothelin receptor type B EDNRB
Endothelin-1 receptor EDNRA

Referensi & Sumber

Synthesis reference: Maurizio TADDEI, Diletta Naldini, Pietro Allegrini, Gabriele Razzetti, Simone Mantegazza, "Process for the Preparation of Bosentan." U.S. Patent US20090156811, issued June 18, 2009.

Contoh Produk & Brand

Produk: 76 • International brands: 0
Produk
  • Accel-bosentan
    Tablet • 125 mg • Oral • Canada • Generic • Approved
  • Act Bosentan
    Tablet • 62.5 mg • Oral • Canada • Approved
  • Act Bosentan
    Tablet • 125 mg • Oral • Canada • Approved
  • Alembic-bosentan
    Tablet • 62.5 mg • Oral • Canada • Approved
  • Alembic-bosentan
    Tablet • 125 mg • Oral • Canada • Approved
  • Apo-bosentan
    Tablet • 62.5 mg • Oral • Canada • Generic • Approved
  • Apo-bosentan
    Tablet • 125.0 mg • Oral • Canada • Generic • Approved
  • Auro-bosentan
    Tablet • 62.5 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 76 produk.

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